Eperezolid |
Catalog No.GC16781 |
Oxazolidinone antibacterial agent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 165800-04-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MIC50: 0.5, 1.0, 2.0, 1.0, 16.0 and 2.0 mg/L for Pcptostreptococcus, Propionibacterium acnes, Ciostridium pefringens, Clostridium dijiicile, Bactrroidesjagilis, and Fusobacterium, respectivley
Anaerobic bacteria are a common cause of serious infections. Anaerobic species which predominate in clinical infections include the Bacteroides fragilis group, Clostridium spp. and Peptostreptococcus spp. The oxazolidinones are a novel class of synthetic antimicrobials inhibiting the initiation of protein synthesis. Two compounds of this class, eperezolid and linezolid have been shown to inhibit Enterococcus faecalis and Enterococcus faecium.
In vitro: Ninety per cent of all tested Propionibacterium acnes (30 strains), PeptostreptococccuJ spp. (50 strains), C. perjringens (50 strains) and C. dficile (50 strains) were inhibited by
In vivo: The in vivo effectiveness of eperezolid and linezolid against one strain each of Enterococcus faecalis and vancomycin-resistant Enterococcus faecium was examined in a rat intraabdominal abscess model. Eperezolid was ineffective at doses of 25 mg/kg of body weight twice daily for the reductions in abscess bacterial density for E. faecalis. Against E. faecium infections, intravenous eperezolid was effective, reducing densities approximately 2 log10 CFU/g [2].
Clinical trials: Oral administration of eperezolid (1 000 mg PO) to healthy volunteers has earlier been reported to yield peak serum concentration of 6.28 mg/L, respectively, while the trough concentration was estimated to be 1.62 mg/L, respectively [3].
References:
[1] Edlund C, Oh H, Nord CE. In vitro activity of linezolid and eperezolid against anaerobic bacteria. Clin Microbiol Infect. 1999;5(1):51-53.
[2] Schülin T, Thauvin-Eliopoulos C, Moellering RC Jr, Eliopoulos GM. Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother. 1999;43(12):2873-6.
[3] Schaadt RD, Batts DH, Daley-Yates PT, Pawsey SD, Stalker DJ, Zurenko GE. Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid. Diagn Microbiol Infect Dis. 1997;28(4):201-4.
Cas No. | 165800-04-4 | SDF | |
Chemical Name | N-[[(5S)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide | ||
Canonical SMILES | CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCN(CC3)C(=O)CO)F | ||
Formula | C18H23FN4O5 | M.Wt | 394.4 |
Solubility | ≥ 14.05mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5355 mL | 12.6775 mL | 25.355 mL |
5 mM | 0.5071 mL | 2.5355 mL | 5.071 mL |
10 mM | 0.2535 mL | 1.2677 mL | 2.5355 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 25 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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